Abstract:
:The agonist, [3H](-)[S]-1-(2-amino-2-carboxyethyl)-5-fluoro-pyrimidine-2,4-dione ([3H](S)F-Willardiine) binding to functional alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors of resealed plasma membrane vesicles and nerve endings freshly isolated from the rat cerebral cortex displayed two binding sites (K(D1)=33+/-7 nM, B(MAX1)=1.6+/-0.3 pmol/mg protein, K(D2)=720+/-250 nM and B(MAX2)=7.8+/-4.0 pmol/mg protein). The drug which impairs AMPA receptor desensitisation, 6-chloro-3,4-dihydro-3-(2-norbornene-5-yl)-2H-1,2,4-benzothiadiazine-7-sulphonamide-1,1-dioxide (cyclothiazide, CTZ) fully displaced the [3H](S)F-Willardiine binding at a concentration of 500 microM. In the presence of 100 microM CTZ (K(I(CTZ))=60+/-6 microM), both the antagonist [3H]-1,2,3,4-tetrahydro-6-nitro-2,3-dioxo-benzo(F)quinoxaline-7-sulfonamide ([3H]NBQX: K(D)=24+/-4 nM, B(MAX)=12.0+/-0.1 pmol/mg protein) and the high-affinity agonist binding showed similar affinity reduction ([3H](S)F-Willardiine: K(D)=140+/-19 nM, B(MAX)=2.9+/-0.5 pmol/mg protein; [3H]NBQX: K(D)=111+/-34 nM, B(MAX)=12+/-3 pmol/mg protein). To disclose structural correlates underlying genuine allosteric binding interactions, molecular mechanics calculations of CTZ-induced structural changes were performed with the use of PDB data on extracellular GluR2 binding domain dimeric crystals available by now. Hydrogen-bonding and root mean square (rms) values of amino acid residues recognising receptor agonists showed minor alterations in the agonist binding sites itself. Moreover, CTZ binding did not affect dimeric subunit structures significantly. These findings indicated that the structural changes featuring the non-desensitised state could possibly occur to a further site of the extracellular GluR2 binding domain. The increase of agonist efficacy on allosteric CTZ binding may be interpreted in terms of a mechanism involving AMPA receptor desensitisation sequential to activation.
journal_name
Neurochem Intjournal_title
Neurochemistry internationalauthors
Kovács I,Simon A,Szárics E,Barabás P,Héja L,Nyikos L,Kardos Jdoi
10.1016/s0197-0186(03)00137-2subject
Has Abstractpub_date
2004-03-01 00:00:00pages
271-80issue
4eissn
0197-0186issn
1872-9754pii
S0197018603001372journal_volume
44pub_type
杂志文章abstract::Individual analysis of synaptic terminals calcium responses, induced by dinucleotides pentaphosphate, Ap(5)A or Gp(5)G, demonstrates the presence of two main groups considering the concentration required for stimulation. The first group corresponds to those responding to Ap(5)A or Gp(5)G at nanomolar concentration, re...
journal_title:Neurochemistry international
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journal_title:Neurochemistry international
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journal_title:Neurochemistry international
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journal_title:Neurochemistry international
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journal_title:Neurochemistry international
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journal_title:Neurochemistry international
pub_type: 杂志文章,评审
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journal_title:Neurochemistry international
pub_type: 杂志文章
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2008.08.006
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2012.03.020
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2003.11.007
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2007.05.018
更新日期:2007-10-01 00:00:00
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journal_title:Neurochemistry international
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2006.03.001
更新日期:2006-09-01 00:00:00
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journal_title:Neurochemistry international
pub_type: 杂志文章
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/0197-0186(87)90032-5
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journal_title:Neurochemistry international
pub_type: 杂志文章,评审
doi:10.1016/j.neuint.2012.05.007
更新日期:2012-07-01 00:00:00
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journal_title:Neurochemistry international
pub_type: 杂志文章
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journal_title:Neurochemistry international
pub_type: 杂志文章
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2011.08.003
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journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2011.08.021
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journal_title:Neurochemistry international
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journal_title:Neurochemistry international
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doi:10.1016/j.neuint.2010.01.010
更新日期:2010-05-01 00:00:00
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journal_title:Neurochemistry international
pub_type: 杂志文章
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abstract::Synaptic like microvesicles (SLMV) form a pleiomorphic population of vesicles present in neuroendocrine cells of the pituitary and the adrenal medulla. Their composition and biogenesis is very similar to small synaptic vesicles (SSV) present in nerve terminals. Membrane proteins of SSV involved in fusion (synaptotagmi...
journal_title:Neurochemistry international
pub_type: 杂志文章,评审
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更新日期:1995-09-01 00:00:00
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journal_title:Neurochemistry international
pub_type: 杂志文章
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journal_title:Neurochemistry international
pub_type: 杂志文章
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abstract::Lipid peroxidation has many deleterious effects on cells, and in the nervous system is considered to be involved in the pathogenesis of neurodegenerative diseases. To suppress lipid peroxidation, cells have various defense systems such as glutathione and thioredoxin, and defects in these defense systems will result in...
journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2010.04.015
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abstract::The expression of 5-hydroxytryptamine-2B (5-HT2B) receptor mRNA has recently been shown in cultured astrocytes. Here the expression of functional 5-HT2B receptors has been studied in cultured astrocytes from rat cerebral cortex, hippocampus, and brain stem. Fluo-3- and fura-2-based microspectrofluorometry was used for...
journal_title:Neurochemistry international
pub_type: 杂志文章
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abstract::In the present study, we investigated the neuroprotective role of p38 inhibition on experimental stroke in rats. p38 inhibition treatment alleviated the brain infarction volume and neurological deficits following ischemia, promoted the activation of Extracellular signal-regulated kinases (ERK1/2), suppressed the activ...
journal_title:Neurochemistry international
pub_type: 杂志文章
doi:10.1016/j.neuint.2015.06.010
更新日期:2015-11-01 00:00:00